Membrane proteins are an essential component of intercellular signaling pathways. The overwhelming majority of small molecule drugs, either directly or indirectly, target membrane proteins. Arrays of membrane proteins would be important tools in drug screening and academic research laboratories in studies of interactions between proteins and lipids, proteins and membrane proteins, as well as therapeutic drugs. Although other microarrays technologies such as DNA and antibody microarrays have been well- developed, membrane protein microarray has been under-developed to fulfill the needs in biomedical research and drug screening. Life BioScience Inc. (LBSI) proposes to develop a commercially viable membrane protein array system capable of studying membrane protein function and interactions in a high multiplexed and high throughput manner by overcoming current technical barriers. Phase I studies will focus on developing microarray platform and validating the general applicability of the platform to produce functional membrane protein arrays. In Phase II we will expand the system to higher multiplex G-protein-coupled receptors (GPCRs) microarrays and incorporate a high sensitivity detection system to comprise a complete membrane protein assay platform for protein functional analysis and drug screening applications. This platform will drastically accelerate investigations of protein-lipid, protein-membrane protein, drug-membrane protein, and drug-membrane interactions, and will be useful in the development and screening of drugs targeting a variety of disease states, including cancer, inflammatory diseases, infectious diseases, heart disease, and kidney disease. PUBLIC HEALTH RELEVANCE: Biological membrane proteins play an important role in all living systems. The proposed research in developing membrane protein arrays addresses important needs in the areas of membrane protein function and drug screening and characterization. The membrane protein arrays will be useful in the development of effective and safe therapeutic agents for the treatment of wide range diseases such as cancer, diabetes, inflammation, and cardiac dysfunction.